Discovery of novel pyrrole derivatives as potent agonists for the niacin receptor GPR109A

https://doi.org/10.1016/j.bmcl.2020.127105Get rights and content
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Abstract

Novel pyrrole derivatives were discovered as potent agonists of the niacin receptor, GPR109A. During the derivatization, compound 16 was found to be effective both in vitro and in vivo. The compound 16 exhibited a significant reduction of the non-esterified fatty acid in human GPR109A transgenic rats, and the duration of its in vivo efficacy was much longer than niacin.

Keywords

GPR109A
Niacin
Pyrrole
Lipolysis
Non-esterified fatty acid

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